Shibnev V A, Finogenova M P, Grinberg L N, Allakhverdiev A M
Bioorg Khim. 1988 Nov;14(11):1565-9.
2-Methoxy-6-chloroacridine-9-yl- and 2-ethoxy-6-nitroacridine-9-yl-hydrazides of glycine, alpha- and beta-alanines, gamma-aminobutiric acid, epsilon-aminocaproic acid have been synthesized and their antimalarial activity has been investigated. The compounds were found to inhibit the growth of malaria parasite P. falciparum in in vitro cultures. Fifty per cent inhibitory concentrations ranged from 2 x 10(-7) to 6 x 10(-7) M and corresponded to therapeutic concentrations of known quinoline and acridine antimalarial drugs. The beta-alanine and gamma-aminobutiric acid derivatives were the most active and showed high activity against a chloroquine resistant strain of P. falciparum.
已合成甘氨酸、α-丙氨酸、β-丙氨酸、γ-氨基丁酸、ε-氨基己酸的2-甲氧基-6-氯吖啶-9-基和2-乙氧基-6-硝基吖啶-9-基酰肼，并对其抗疟活性进行了研究。发现这些化合物在体外培养中能抑制恶性疟原虫的生长。50%抑制浓度范围为2×10⁻⁷至6×10⁻⁷ M，与已知喹啉和吖啶抗疟药物的治疗浓度相当。β-丙氨酸和γ-氨基丁酸衍生物活性最高，对氯喹耐药的恶性疟原虫菌株表现出高活性。
